The Synthesis And Research Of Rosuvastatin Calcium

Rosuvastatin calcium,which chemical name is(3R,5S,6E)-7-[4-(4-fluorophe nyl)-6-(1-methylethyl)-2-[N-methyl(N-methylsulfonyl)amino]-5-pyrimidinyll]-3,5-dih ydroxy-6-Heptenoic calcium(Trade name called "Crestor"),is a fully synthetic single enantiomorphism isomer of a new generation of statins,due to its safety and efficiency,it is known as "super statin".Its preparation technology receives more and more attention.In this paper,4-(4-Fluorophenyl)-6-isopropyl-2-[(N-methyl-N-methylsulfonyl)amino]pyrimidine-5-yl-formyl(Z8.1)and Methyl(3R)-3-(tert-butyldimethylsilylox y)-5-oxo-6-triphenylphosphoranylidene hexanoate(J6)as starting material,after Wittig reaction,deprotection,chiral reduction,hydrolysis into salt purification,free to obtain rosuvastatin calcium(3R,5S,6E)-7-[4-(4-fluorophenyl)-6-(1-methyle thyl)-2-[N-methyl(N-methylsulfonyl)amino]-5-pyrimid:inyl]-3,5-dihydroxy-6-Hepten oiccalcium(ROZ-7).Wittig reaction of the synthesis process is optimized to get the appropriate solvent and materiel proportioning;the reaction conditions of the deprotection is studied,a mild,cheap hydrofluoric acid solution is used to deprotect.The conditions of chiral reduction reaction and salt purification were reviewed,finally,the cheap and readily available isopropyl amine is selected as the reagent for salt purification.At last,free to get rosuvastatin calcium,the total molar yield of rosuvastatin calcium is as high as 76.3%under the optimal reaction condition.Meanwhile,the work of characterization of Rosuvastatin calcium has been performed by elemental analysis?IR?UV?NMR?MS.